Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.

doi:10.1158/1535-7163.MCT-11-0474

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.

Molecular cancer therapeutics - 1 Feb 2012

Maira Sauveur-Michel, Pecchi Sabina, Huang Alan, Burger Matthew, Knapp Mark, Sterker Dario, Schnell Christian, Guthy Daniel, Nagel Tobi, Wiesmann Marion, Brachmann Saskia, Fritsch Christine, Dorsch Marion, Chène Patrick, Shoemaker Kevin, De Pover Alain, Menezes Daniel, Martiny-Baron Georg, Fabbro Doriano, Wilson Christopher J, Schlegel Robert, Hofmann Francesco, García-Echeverría Carlos, Sellers William R, Voliva Charles F

Abstract excerpt

Following the discovery of NVP-BEZ235, our first dual pan-PI3K/mTOR clinical compound, we sought to identify additional phosphoinositide 3-kinase (PI3K) inhibitors from different chemical classes with a different selectivity profile. The key to achieve these objectives was to couple a structure-based design approach with intensive pharmacologic evaluation of selected compounds during the medicinal chemistry...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Aminopyridines

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Biological Availability

Share to HCT116 Cells

Share to HT29 Cells

Share to Morpholines

Share to Phosphatidylinositol 3-Kinase

Share to Phosphoinositide-3 Kinase Inhibitors

Share to Tumor Burden

Source

Open in PubMed

Identifiers

PMID: 22188813
DOI: 10.1158/1535-7163.MCT-11-0474

Genes

KRAS
PTEN

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.PMID 22188813Read ↗

Antitumor Activity of NVP-BKM120—A Selective Pan Class I PI3 Kinase Inhibitor Showed Differential Forms of Cell Death Based on p53 Status of Glioma CellsSemantic proximity Read ↗

WJD008, a dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin inhibitor, prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant.Semantic proximity Read ↗

Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug designSemantic proximity Read ↗

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).Semantic proximity Read ↗

Phosphatidylinositol 3-kinase (PI3K) inhibitors: a recent update on inhibitor design and clinical trials (2016-2020).Semantic proximity Read ↗

Current State and Future Challenges for PI3K Inhibitors in Cancer TherapySemantic proximity Read ↗

Functional Characterization of an Isoform-Selective Inhibitor of PI3K-p110β as a Potential Anticancer AgentSemantic proximity Read ↗

Challenges in the clinical development of PI3K inhibitors.Semantic proximity Read ↗

BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110α and p110δ Activities in Tumor Cell Lines and Xenograft ModelsSemantic proximity Read ↗

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the ClinicSemantic proximity Read ↗

Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual InhibitorsSemantic proximity Read ↗

Picking the Point of Inhibition: A Comparative Review of PI3K/AKT/mTOR Pathway InhibitorsSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.